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Submit ReviewDihydroergotoxine mesylate
Description: Binds to GABAA receptor Cl- channel; allosteric modulator of benzodiazepine site
Biological Activity for Dihydroergotoxine mesylate
Dihydroergotoxine mesylate is a complex of closely related alkaloid salts. Binds with high affinity to the GABAA receptor Cl- channel, producing an allosteric interaction with the benzodiazepine site. Also interacts with central dopaminergic, serotonergic and adrenergic (α1) receptors. Displays antiproliferative activity in vitro (IC50 = 18 - 38 μM in prostate cancer cells) and exhibits cognition-enhancing, anticonvulsant and sedative activity in vivo. Orally active.
Technical Data for Dihydroergotoxine mesylate
| Storage | Store at RT |
| CAS Number | 8067-24-1 |
| PubChem ID | 92044435 |
| InChI Key | HMMYROQEJAZVGJ-CTOOOFERSA-N |
| Smiles | [H][C@]4([C@@]([H])3C[C@@H]([C@@](N[C@@]5([C@H](C)C)C(N([C@@]([H])([C@@H](C)C)C(N7[C@]([H])6CCC7)=O)[C@@]6(O)O5)=O)=O)CN4C)CC1=CNC2=C1C3=CC=C2.[H][C@]%11([C@@]([H])%10C[C@@H]([C@@](N[C@@]%12([C@H](C)C)C(N([C@@]([H])(CC%15=CC=CC=C%15)C(N%14[C@]([H])%13CCC%14)=O)[C@@]%13(O)O%12)=O)=O)CN%11C)CC8=CNC9=C8C%10=CC=C9.[H][C@]%19([C@@]([H])%18C[C@@H]([C@@](N[C@@]%20([C@H](C)C)C(N([C@@]([H])(CC(C)C)C(N%22[C@]([H])%21CCC%22)=O)[C@@]%21(O)O%20)=O)=O)CN%19C)CC%16=CNC%17=C%16C%18=CC=C%17.[H][C@]%26([C@@]([H])%25C[C@@H]([C@@](N[C@@]%27([C@H](C)C)C(N([C@@]([H])([C@@H](CC)C)C(N%29[C@]([H])%28CCC%29)=O)[C@@]%28(O)O%27)=O)=O)CN%26C)CC%23=CNC%24=C%23C%25=CC=C%24.CS(=O)(O)=O.CS(=O)(O)=O.CS(=O)(O)=O.CS(=O)(O)=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Product Datasheets for Dihydroergotoxine mesylate
References for Dihydroergotoxine mesylate
References are publications that support the biological activity of the product.
Abdul et al (2008) Expression of gamma-aminobutyric acid receptor (subtype A) in prostate cancer Acta Oncol. 47 1546 PMID: 18607852
Tvrdeic and Perici (1991) Dihydrogenated ergot compounds bind with high affinity to GABAA receptor-associated Cl- ionophore. Eur.J.Pharmacol. 202 109 PMID: 1664802
Tvrdeic and Perici (1992) Dihydroergotoxine modulation of the GABAA receptor-associated Cl- ionophore in mouse brain. Eur.J. Pharmacol. 221 139 PMID: 1333969
Tvredic and Perici (2003) Effects of ergot alkaloids on 3H-flunitrazepam binding to mouse brain GABAA receptors. Coll.Antropol. 27 S175 PMID: 12955907
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Keywords: Dihydroergotoxine mesylate, Dihydroergotoxine mesylate supplier, Binds, GABAA, receptor, Cl-, channel, allosteric, modulators, benzodiazepine, site, Receptors, 0505, Tocris Bioscience
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Literature in this Area
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